Brands, Medical Use, Clinical Data
- Anti-Inflammatory Agents, Non-Steroidal
- Cyclooxygenase Inhibitors
- Tablet (oral, equivalent to 200 mg or 600 mg of tolmetin)
- Capsule (oral, equivalent to 400 mg of tolmetin)
Brands / Synonyms
Tolectin; Tolectin DS; Tolmetin; Tolmetin Sodium; Tolmetin [USAN:BAN:INN]; Tolmetina [DCIT]; Tolmetine; Tolmetine [INN-French]; Tolmetino [INN-Spanish]; Tolmetinum; Tolmetinum [INN-Latin]
For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis, including the treatment of acute flares long-term management. Also for treatment of juvenile rheumatoid arthritis.
Tolmetin is a nonsteroidal anti-inflammatory agent. Studies in animals have shown tolmetin to possess anti-inflammatory, analgesic and antipyretic activity. In the rat, tolmetin prevents the development of experimentally induced polyarthritis and also decreases established inflammation. In patients with either rheumatoid arthritis or osteaoarthritis, tolmetin is as effective as aspirin and indomethacin in controlling disease activity, but the frequency of the milder gastrointestinal adverse effects and tinnitus was less than in aspirin-treated patients, and the incidence of central nervous system adverse effects was less than in indomethacin-treated patients. In patients with juvenile rheumatoid arthritis, tolmetin is as effective as aspirin in controlling disease activity, with a similar incidence of adverse reactions. tolmetin has produced additional therapeutic benefit when added to a regimen of gold salts and, to a lesser extent, with corticosteroids. Tolmetin should not be used in conjunction with salicylates since greater benefit from the combination is not likely, but the potential for adverse reactions is increased.
Mechanism of Action
The mode of action of tolmetin is not known. However, studies in laboratory animals and man have demonstrated that the anti-inflammatory action of tolmetin is not due to pituitary-adrenal stimulation. Tolmetin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action. Tolmetin does not appear to alter the course of the underlying disease in man.
Rapidly and almost completely absorbed with peak plasma levels being reached within 30-60 minutes after an oral therapeutic dose.
Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain.
Biotrnasformation / Drug Metabolism
Essentially all of the administered dose is recovered in the urine in 24 hours either as an inactive oxidative metabolite or as conjugates of tolmetin.
Anaphylactoid reactions have been reported with TOLECTIN as with other nonsteroidal anti-inflammatory drugs.
Because of the possibility of cross-sensitivity to other nonsteroidal anti-inflammatory drugs, particularly zomepirac
sodium, anaphylactoid reactions may be more likely to occur in patients who have exhibited allergic reactions to
these compounds. For this reason, TOLECTIN should not be given to patients in whom aspirin and other nonsteroidal
anti-inflammatory drugs induce symptoms of asthma, rhinitis, urticaria and other symptoms of allergic or
anaphylactoid reactions. Patients experiencing anaphylactoid reactions on TOLECTIN should be treated with
conventional therapy, such as epinephrine, antihistamines and/or steroids.
The in vitro binding of warfarin to human plasma proteins is unaffected by tolmetin, and tolmetin does not
alter the prothrombin time of normal volunteers. However, increased prothrombin time and bleeding have been reported
in patients on concomitant TOLECTIN and warfarin therapy. Therefore, caution should be exercised when administering
TOLECTIN to patients on anticoagulants.
In adult diabetic patients under treatment with either sulfonylureas or insulin there is no change in the clinical
effects of either TOLECTIN or the hypoglycemic agents.
Caution should be used if TOLECTIN is administered concomitantly with methotrexate. TOLECTIN and other
nonsteroidal anti-inflammatory drugs have been reported to reduce the tubular secretion of methotrexate in an animal
model, possibly enhancing the toxicity of methotrexate.
Because serious GI tract ulceration and bleeding can occur without warning symptoms, physicians should follow
chronically treated patients for the signs and symptoms of ulceration and bleeding and should inform them of the
importance of this follow-up.